Literature DB >> 18947993

In situ blood-brain barrier permeability of a C-10 paclitaxel carbamate.

Carlo Ballatore1, Bin Zhang, John Q Trojanowski, Virginia M-Y Lee, Amos B Smith.   

Abstract

We report the synthesis and blood-brain barrier (BBB)-permeability of (14)C-CNDR-29, a paclitaxel C-10 carbamate derivative shown to be devoid of P-glycoprotein (Pgp)-interactions, in an in situ mouse brain perfusion model, in comparison with (14)C-paclitaxel. The results presented reveal a 3- to 4-fold higher BBB-permeability for the C-10 modified taxane compared to paclitaxel. These results support the notion that circumvention of Pgp-mediated efflux can lead to higher BBB-permeability. Further studies however are needed to evaluate the therapeutic potential of the C-10 carbamates paclitaxel derivatives for the treatment of CNS diseases.

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Year:  2008        PMID： 18947993      PMCID： PMC2603177          DOI： 10.1016/j.bmcl.2008.10.024

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  14 in total

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3.  A facile route to paclitaxel C-10 carbamates.

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Journal:  Bioorg Med Chem Lett       Date:  2005-05-16       Impact factor: 2.823

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Review 5.  The blood-brain barrier in health and chronic neurodegenerative disorders.

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7.  Chemical modification of paclitaxel (Taxol) reduces P-glycoprotein interactions and increases permeation across the blood-brain barrier in vitro and in situ.

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8.  Increased penetration of paclitaxel into the brain by inhibition of P-Glycoprotein.

Authors:  E Marleen Kemper; A Erik van Zandbergen; Cindy Cleypool; Henk A Mos; Willem Boogerd; Jos H Beijnen; Olaf van Tellingen
Journal:  Clin Cancer Res       Date:  2003-07       Impact factor: 12.531

9.  The effect of P-glycoprotein on paclitaxel brain and brain tumor distribution in mice.

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Journal:  Cancer Res       Date:  2003-08-15       Impact factor: 12.701

Review 10.  Paclitaxel (taxol)

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Journal:  N Engl J Med       Date:  1995-04-13       Impact factor: 91.245
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Review 3.  Back to the tubule: microtubule dynamics in Parkinson's disease.

Authors:  Laura Pellegrini; Andrea Wetzel; Simone Grannó; George Heaton; Kirsten Harvey
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  3 in total

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